Monday, March 11, 2013

URSODEOXYCHOLIC ACID



Ursodeoxycholic acid is also known as Ursodiol  and the abbreviation UDCA, is one of the secondary bile acids, which are metabolic byproducts of intestinal bacteria.


3α,7β-dihydroxy-5β-cholan-24-oic acid
OR
(R)-4-((3R,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-
10,13-dimethylhexadecahydro-
1H-cyclopenta[a]phenanthren-17-yl)pentanoic acid

Formula  -  C24H40O4
Mol. mass  -  392.56 g/mol


Endogenous effects

Primary bile acids are produced by the liver and stored in the gall bladder. When secreted into the intestine, primary bile acids can be metabolized into secondary bile acids by intestinal bacteria. Primary and secondary bile acids help the body digest fats. Ursodeoxycholic acid helps regulate cholesterol by reducing the rate at which the intestine absorbs cholesterol molecules while breaking up micelles containing cholesterol. Because of this property, ursodeoxycholic acid is used to treat (cholesterol) gallstones non-surgically.
While some bile acids are known to be colon tumor promoters (e.g. deoxycholic acid), others such as ursodeoxycholic acid are thought to be chemopreventive, perhaps by inducing cellular differentiation and/or cellular senescence in colon epithelial cells.
It is believed to inhibit apoptosis.
Ursodeoxycholic acid has also been shown experimentally to suppress immune response such as immune cell phagocytosis. Prolonged exposure and/or increased quantities of systemic (throughout the body, not just in the digestive system) ursodeoxycholic acid can be toxic.


Pharmaceutical USE

Ursodeoxycholic acid is marketed under the trade names Actigall, Ursosan, Ursofalk, BILIVER, Egyurso, Urso, Urso Forte, Deursil and Coric.
Ursodeoxycholic acid can be chemically synthesized and was brought to market by the Montreal-based Axcan Pharma in 1998, which continues to market the drug.
The drug reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones in patients who want an alternative to surgery. The drug is very expensive, however, and if the patient stops taking it, the gallstones tend to recur if the condition that gave rise to their formation does not change. For these reasons, it has not supplanted surgical treatment by cholecystectomy.
It is the only FDA approved drug to treat primary biliary cirrhosis.
A Cochrane review to evaluate if ursodeoxycholic acid has any beneficial effect in primary biliary cirrhosis patients included 16 randomized clinical trials with a total of 1447 patients. The primary outcome measures were mortality and mortality or liver transplantation. Although treatment with ursodeoxycholic acid showed a reduction in liver biochemistry, jaundice, and ascites, it did not decrease mortality or liver transplantation.
In absence of biochemical response to 13-15mg/kg/day ursodeoxycholic acid, its use is associated with an incidence of 20% hepatocellular carcinoma in patients with primary biliary cirrhosis in 15 years.
In children, its use is not licensed, as its safety and effectiveness are not established.
In double the recommended daily dose ursodeoxycholic acid reduces elevated liver enzyme levels in patients with primary sclerosing cholangitis, but its use was associated with an increased risk of serious adverse events (the development of cirrhosis, varices, death or liver transplantation) in patients who received ursodeoxycholic acid compared with those who received placebo). After adjustment for baseline stratification characteristics, the risk was 2.1 times greater for death,transplantation, or minimal listing criteria in patients on ursodeoxycholic acid than for those on placebo (P = 0.038). Serious adverse events, were more common in the ursodeoxycholic acid group than the placebo group
Research by the Imperial College London has produced promising results in the treatment of arrhythmia, both in patients who have suffered a heart attack and in foetuses, by using ursodiol to change the electrical properties of myofibroblast cells. Myofibroblasts disrupt the transmission of electrical signals controlling heart rhythm.


SOURCE
The drug is generally not derived from animals.However, it is believed up to 10,000 bile bears are kept on farms in China, Vietnam and South Korea for the purpose of harvesting ursodeoxycholic acid. Ursodeoxycholic acid is found in large quantities in bear bile.




Indication & Dosage
Dissolution of cholesterol-rich gallstones
Adult: 6-12 mg/kg daily as a single dose at bedtime or in 2-3 divided doses continued for 3-4 mth after radiological disappearance of stones. Doses may be divided unequally with a higher dose given before bedtime to counteract increase in biliary cholesterol saturation which occurs in early morning. Max: 15 mg/kg.

Hepatic impairment:Chronic liver disease (except primary biliary cirrhosis): use with caution.


Primary biliary cirrhosis
Adult: 10-15 mg/kg daily in 2-4 divided doses.


Prophylaxis of gallstones in patients undergoing rapid weight loss
Adult: 300 mg bid.
Hepatic impairment: Chronic liver disease (except primary biliary cirrhosis): use with caution.


DRUG INTERACTIONS
Cholestyramine, charcoal and antacids may reduce effectiveness. Aluminum-based antacids may reduce absorption. Oestrogens and clofibrate may counteract effectiveness of ursodeoxycholic acid by increasing cholesterol elimination in bile. Possible increase in ciclosporin serum concentration. Decreased effectiveness of dapsone. Possible decrease in serum ciprofloxacin and nitrendipine.


Mechanism of Action     
Ursodeoxycholic acid suppresses hepatic synthesis and secretion of cholesterol and also inhibits intestinal absorption of cholesterol.
Absorption: Rapidly and completely absorbed from the GI tract.
Distribution:Protein binding: 96-98%. Undergoes enterohepatic recycling.
Metabolism:Partly conjugated in the liver before being excreted into the bile. Free and conjugated forms undergo 7a-dehydroxylation to lithocholic acid under the influence of gut bactera. Some are reabsorbed and then further conjugated and sulfated by the liver.
Excretion:Faeces.


Brand Names

Acido Ursodesossicolico Actavis
Actavis Italy, Italy

Acido Ursodesossicolico Angenerico
Angenerico, Italy

Acido Ursodesossicolico Doc
DOC Generici, Italy

Acido Ursodesossicolico Dorom
Dorom, Italy

Acido Ursodesossicolico EG
EG, Italy

Acido Ursodesossicolico Mylan
Mylan, Italy

Acido Ursodesossicolico ratiopharm
ratiopharm Italia, Italy

Acido Ursodesossicolico Winthrop
Winthrop Ph.Italia, Italy

Actigall
Novartis, New Zealand; Watson, United States

Adursal
Leiras, Finland

Audecol
Ariston, Argentina

Bilenor (Ursodeoxycholic Acid and Chenodeoxycholic Acid)
Myung Moon, South Korea

Bilifalk
Dr Falk, Spain

Buraue
Yoshindo, Japan

Canlin
Everest, Taiwan

Choleron
Aversi, Georgia

Cholit-Ursan
STADA, Germany

Choludexan
Sigma, Georgia

Cisbile
Winston, Taiwan

Clotipide
AC Farma, Peru

Coleretik
Sherfarma, Peru

Daewoongursa
Daewoong, Vietnam

Delursan
Axcan, France

Desoxil
Crinos, Italy

Destolit
Norgine, United Kingdom; Sanofi-Aventis, Portugal

Deursil
Sanofi-Aventis, Italy

De-ursil
Sanofi-Aventis, Switzerland

De-ursil RR
Sanofi-Aventis, Switzerland

De-ursil RR mite
Sanofi-Aventis, Switzerland

Dexo
Dominguez, Argentina

Estazor
Fahrenheit, Indonesia

Fraurs
Francia Farmaceutici, Italy

Genurso
Genovate, Taiwan

Legan
Chin Teng, Taiwan

Liconor
Opsonin, Bangladesh

Ligat
TTY Biopharm, Taiwan

Lipo
Gentle, Taiwan

Lithofalk (Ursodeoxycholic Acid and Chenodeoxycholic Acid)
Falk, Germany

Litoff
Caber, Italy

Litomen
Best, Colombia

Litursol
Crinos, Italy

PMS-Ursodiol C
Pharmascience, Canada

Precoat
Tatsumi Kagaku, Japan

Proursan
Pro.Med., Poland

Reptor
Fuso Pharmaceutical, Japan

Sodan
Chen Ho, Taiwan

Solutrat
Sandoz, Argentina

Tantosan
Newai Chem, Taiwan

Ubiron
Medisa Shinyaku, Japan

UDC AL
Aliud, Germany

UDC HEXAL
Hexal, Germany

UDCA Ferring
Ferring, Argentina

Udihep
Win-Medicare, India; Win-Medicare, Thailand

Udihep Forte
Win-Medicare, India

Udoxyl
Ind-Swift, India

Uliden
Swiss Pharm, Taiwan

Urchil
Aamorb, India

Urchil Forte
Aamorb, India

Urdafalk
Darya-Varia, Indonesia; Falk, Indonesia

Urdahex
Kalbe, Indonesia

Urdenacin
Taiyo Pharmaceutical, Japan

Urdes
Errekappa Euroterapici, Italy

Urdeston
Towa Yakuhin, Japan

Urdex
Towa Yakuhin, Japan

Urdox
CP, Malta; Wockhardt, United Kingdom

Urose
Hwang's, Taiwan

Uroso
Johnson, Taiwan

Urosofalk
Dr. Falk, Portugal

Ursa 200MG
Daewoong, Vietnam

Ursa
Dae Woong, South Korea; Daewoong, Thailand

Ursacol
Zambon, Brazil; Zambon, Colombia; Zambon Italia, Italy

Ursidesox
Duncan, Argentina

Ursilon
IBI, Italy

Urso Forte
Aptalis, United States

Urso Heumann
Heumann, Germany

Urso
Aptalis, United States; Axcan, Canada; Mitsubishi Tanabe Pharma, Hong Kong; Mitsubishi-Tokyo, Taiwan; Tanabe Mitsubishi Pharma, Japan

Urso DS
Axcan, Canada

Ursobil
ABC Farmaceutici, Georgia; ABC Farmaceutici, Italy

Ursobilane
Estedi, Spain

Ursocam
Polfarmex, Poland

Ursocel
ABL Pharma, Peru

Ursochol
Zambon, Belgium; Zambon, Switzerland; Zambon, Germany; Zambon, Spain; Zambon, Indonesia; Zambon, Netherlands

Ursocid
Ta Fong, Taiwan

Ursodeoxycholic acid Zensei
Zensei Yakuhin, Japan

Ursodeoxycholic Acid-Daewoong Pharm
Daewoong Pharmaceutial Co. Ltd, China

Ursodeoxycholic Acid-Sunve Pharm
Sunve, China

Ursodeoxycholzuur Imphos
Imphos, Netherlands

Ursodesoxycholic Acid
Ying Yuan, Taiwan

Ursodil
General Pharma, Bangladesh

Ursodiol CorePharma
CorePharma, United States

Ursodiol Epic Pharma
Epic Pharma, United States

Ursodiol Glenmark
Glenmark, United States

Ursodiol Lannett
Lannett, United States

Ursodiol Mylan
Mylan, United States

Ursodiol RR Zentiva
Sanofi-Aventis, Switzerland

Ursodiol Teva
Teva, United States

Ursodiol Watson
Watson, United States

Ursodiol Zentiva
Sanofi-Aventis, Switzerland

Ursodiol
HLB, Argentina

Ursodox
Signova, India

Ursofalk
Farmasa, Mexico; ARIS, Turkey; Biotoscana, Chile; Biotoscana, Colombia; Biotoscana, Peru; Cevallos, Argentina; Codali, Belgium; Codali, Luxembourg; Dr Falk, Hong Kong; Dr. Falk, Israel; Dr. Falk, Norway; Dr. Falk, Russian Federation; Dr. Falk Pharma, Czech Republic; Dr. Falk Pharma, Serbia; Eureco, Netherlands; Falk, Bosnia & Herzegowina; Falk, China; Falk, Germany; Falk, United Kingdom; Falk, Hungary; Falk, Ireland; Falk, Lithuania; Falk, Malta; Falk, Philippines; Falk, Poland; Falk, Romania; Falk, Singapore; Falk, Slovakia; Falk, Thailand; Falk Pharma GmbH, Latvia; Farmak, Estonia; Galenica, Greece; IFET, Greece; Meda, Sweden; Merck, Austria; Orphan, Australia; Salus, Slovenia; Schwabe, Costa Rica; Schwabe, Guatemala; Schwabe, Honduras; Schwabe, Panama; Schwabe, El Salvador; Tramedico, Netherlands; Vifor, Switzerland; Würth, Croatia (Hrvatska); Zydus Cadila, India


Ursoflor
So.Se. Pharm, Italy

Ursogal
Galen, United Kingdom

Ursol
Siu Guan, Taiwan

Ursolic
Gentle, Taiwan; Guardian Pharmatama, Indonesia

Ursolin
Berlin, Thailand

Ursolisin
Magis, Italy

Ursolit
CTS, Israel

Ursolvan
Sanofi-Aventis, France

Ursomac
GMP, Georgia

Ursomax
Altius, Argentina

Ursophalc
Falk, Georgia

Ursopol
ICN, Poland

Ursosan
Evolan, Sweden; Pro.Med.CS, Bosnia & Herzegowina; Pro.Med.CS, Czech Republic; Pro.Med.CS, Estonia; Pro.Med.CS, Georgia; Pro.Med.CS, Lithuania; Pro.Med.CS, Romania; Pro.Med.CS, Serbia; Pro.Med.CS, Slovenia; Pro.Med.CS, Slovakia


Ursotan
Sanofi-Aventis, South Africa

Ursultec
Otifarma, Italy

Urzac
Quesada, Argentina

Usol
Shyh Dar, Taiwan


















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